Transcript alberto-ritieni-university-of-naples-federico-ii

Università degli Studi di Napoli Federico II
Dipartimento di Farmacia
Nutraceutical potential of artichoke
(Cynara scolymus) edible and waste portions
25 September 2014
Prof. Dr. H.c. Alberto Ritieni
Prof. Dr. H.c. Alberto Ritieni
Phone +39-081-678.652
e-mail [email protected]
Fax +39-081-678.610 Mobile +39-393-68.55.043
“Health is a state of complete
physical, mental and social,
and not merely the absence of
disease”
(OMS, 1947)
How has lengthened the average life of industrialized populations?
Life expectancy in
years
“Health is a state of complete
physical, mental and social, and not
merely the absence of disease…
+
…the maintenance of the state of wellbeing and pleasure to be nice and accept”
Current Scenario
61.3% of the population claims to be in good health
male
female
2 years more of life in a single decade
The solution isn’t to “add years to
life” but is important to
“add life and quality to years”
Life expectancy
Life quality
How to prevent diseases ????
DNA capital from parents
Surgical
emergency
Environment
Lifestyles
(Nutrition)
Health Status
Innovative Pharmacotherapy
…drugs for health people
Suggested for the treatment of risk factors that
result from improper lifestyles or conditions
NOT ONLY pathological that produce restictions
on the welfare of persons
How to prevent disease ????
Drugs
Nutraceuticals
Expect the expression
of the disease
Phase of the attack
is the best defense
FUNCTIONAL FOOD AND
NUTRACEUTICALS
FUNCTIONAL FOODS
Foods characterized by additional effects due
to the presence of components naturally
present or added which interact more or less
selectively with one or more physiological
functions of the organism, leading to positive
effects on the maintenance of health and / or
prevention of diseases.
Dietary Supplements
Foods that supplement the diet and
are formulated with vitamins and
minerals, or other substances with
nutritional and / or physiological
effects. Include: amino acids,
essential fatty acids, fiber and plantderived extracts and can be dosed
alone or in combination.
Nutraceutical
It was in Rome that in 1989 Stephen De Felice,
medical, founder and President of the Foundation
for Innovation in Medicine coined the term
nutraceutical by "nutrition” and "pharmaceutical"
According to the original definition, the nutraceutical may be
considered, "a food (or part of the food), which gives beneficial effects
to health (principle medicated), including the prevention and / or
treatment of a disease ”
Food supplements
Functional
Food
Nutraceutical
“drug and food”
“beyond diet, before drug”
Garlic
Artichoke
Onion
Potato
Tomato
Vitamin C
Carotenoids
Phosphorus
Calcium
Kalium
Sodium
Fiber
Lipid
Chemical composition and nutritional asset of several vegetables (100 g)
Simple phenols and oligomers isolated by food
sources
Artichoke
• The artichoke (Cynara scolimus L.) belongs to the family
of Astraceae, a former family Compositae.
• The genus is most interesting is the Cynara which includes eight
wild species all originating from the Mediterranean basin
discoveries in the fifteenth and sixteenth centuries.
It is a rhizomatous
herbaceous plant which has
an inflorescence is
protected by bracts which,
together with the basal
portion, tender, are the
edible part
Artichoke
• In Italy there are 50,000 hectares cultivated
and are produced over 500,000 tonnes (40%
of world production).
• Italy is the first country in the world
producer of artichokes
• Apulia is the first Region in Italy 36,3% of
hectars, Sicily (28,4%), Sardinia (21,4%),
Campania (5,6%), Lazio (2,5%) and Tuscan
(2%)
Artichoke
Artichoke and Nutrients
Water
86%
Proteins
2%
Lipids
0.2
Glucids
Soluble (glucose)
12.5%
2.0
Energy
42 kcal
Vitamins
B1, B2, PP
Mineral Salts K+ , Na+, Ca 2+ Fe3+
Artichoke and Bioactive Metabolites
• From artichoke have been isolated a large group
of polyphenols. The main components are
Chlorogenic Acid, Cynarin and Caffeic Acid
(obtained by hydrolysis of Cynarin and
Chlorogenic Acid)
In the extracts are present numerous
diphenols and bioactive flavanoids
Main bioctive compounds of Artichoke
Chlorogenic Acids
• 5-O-caffeylchinico Acid
• 1,5-dicaffeylchinico Acid
• Caffeic Acid
Extract of Cynara
Flavonoids
• Luteolin
• Cynaroside
• Scolimoside
POLYPHENOLIC COMPOUNDS
HYDOXYCINNAMATES
FLAVONOIDS
Apigenin
Quinic acid
Cynarin
Chlorogenic acid
Luteolin
Main bioctive compounds of Artichoke
Amount of compounds in ppm
Chlorogenic Acid
Hydrophilic
extract
262.7
Mono-caffeoylquinic Acid
496.0
Cynarin
42.0
Luteolin 7-O-rutinoside
47.9
Luteolin 7-O-glucoside
14.0
Luteolin 7-O-malonil glucoside
8.5
Luteolin
2.9
Di-caffeoylquinico
46.0
Polyphenols Total
920.7
Chlorogenic Acid
Chlorogenic Acid
Potential Nutraceutical activities of
Artichoke’s extracts
They marked in vitro and in vivo hepatoprotective
effects, choleretic and hypocholesterolemic
In '900 scientific
research focuses on the
properties "hepato
stimulant” leaf extracts
of Cynara, advocated
by doctors' 700.
Main mode of actions of the extracts of
Cynara scolymus
Antioxidant Activity
The dry extract of leaves of artichoke
protects the liver from damage caused by
hepatotoxic CCl4 as the hydroxide, cumene
and tert-butyl-hydroperoxide
The components which
perform the antioxidant are
the phenolic acids like:
Cynarin and Caffeic acid
Nutraceutical Potential Power
• Antioxidant Power
• Antimicrobical Activity
• Cell Tests: antitumoral activity, potential
hypoglycemic, lipid-lowering potential
• Bioaccessibility and bioavailability
Potential activities of Cynara Scolymus
Anti-HIV
Antifungal
McDougall, B., King, P. J., Wu, B. W., Hostomsky, Z.,
Manfred, G., & Robinson, W. E. Jr., (1998)
Zhu, X. F., Zhang, H. X., & Lo, R. (2005)
Antioxidant Source
Brown, J. E.; Rice-Evans, C.
Anticarcinogenic
Michael N Clifford
Hepatoprotective
TOMASA DZET,J ORGE CAMARASAa, nd JUAN CARLOSL AGUNA+
Antibacterial
Diuretic
anti-inflammatory
CHOLESTEROL-LOWERING
AND HYPOGLYCEMIC
Clifford, M.; Walker, R.
Heidarian, Esfandiar; Soofiniya, Yadollah
Artichoke by-products
Very reach sources
or bioactive
metabolites
Quali-quantitative analysis of
Artichoke extracts
1.Extraction of samples with different protocols
2.Purification of bioactive metabolites by HPLC, MPLC, etc.
3.Chemical Identification of bioactive metabolites by mass
spexctrometry, NMR etc.
Relative pure extracts
Chlorgenic Acid Quantification
Artichoke
mg AC/100 g
Romolo stem
27,826
Romolo heads
6,276
Romolo leaves
0,5
Antioxidant Activity Evaluation
Artichoke
Romolo stem
Romolo heads
Romolo leaves
Total Phenols
Content
mg AGE/100 g
DPPH
μmolTE/100 g
FRAP μmolTE/
100 g
21,35
4,53
26,44
78,61
38,95
124,47
104,46
24
64,54
HPLC run of the extract of Artichoke
Chlorogeni
c Acid
Voltage
Neo Chlorogenic
Acid
Crypto
Chlorogenic Acid
Time
UHPLC-PDA chromatogram of Cynara Scolymus heads polyphenolic extract . Peaks identified are: (1): Syringic acid O-hexoside;
(2): Trihydroxyoctadecenoic acid;
(3): Dicaffeoylquinic acid;
(4): Monocaffeoylquinic Acid;
(5): Propadienoic acid;(6):
Dicaffeoylquinic acid (isomer I); (7): Apigenin-7-O-glucoside; (8): Propadienoic acid; (9): p-Coumarylglucoside; (10): Apigenin-7O-cinnamoylglucoside; (11): 1-Hydroxypinoresinol 1-o-β-D-glucoside; (12): Unknown; (13): 3-O-Feruloylquinic acid; (14): 3-OFeruloylquinic acid (isomer); (15): Lusitanicoside (chavicol β rutinoside); (16): Luteolin-7-O-glucoside (Cynaroside); (17):
Isorhamnetin 3-o-rhamnoside; (18): Lusitanicoside(Chavicol β-rutinoside) (isomer); (19) :Unknown; (20): Pinoresinol-4-O βglucoside; (21): Dicaffeoylquinic acid (isomer II); (22): Dicaffeoylquinic acid (isomer III); (23): Isorhoifolin (Apigenin-7-O-rutinoside);
(24): Isoquercitrin;
(25): Apigenin-7-O-glucuronide; (26): Apigenin-7-O-glucoside (isomer); (27): Luteolin-7-O-rutinoside
(scolymoside); (28): Kaempferol 3-o-acetyl glucoside; (29): Pinoresinol-acetylhexoside; (30): Apigenin-7-O-glucuronide (isomer);
(31): Diferuloylquinic acid; (32): Apigenin-7-O-(6’acetyl)glucoside; (33): Luteolin; (34): Hydroxy-octadecatrienoic acid; (35):
Apigenin; (36): Dihydroxypropionhend-hexoside; (37): Trihydroxyoctadecenoic acid.
UHPLC-PDA chromatogram of Cynara Scolymus stems polyphenolic extract. Peaks identified are: (1):
Monocaffeoylquinic acid ; (2): Monocaffeoylquinic acid (isomer); (3): 3-p-Coumarylquinic acid; (4):pCoumaroylquinic acid; (5):Luteolin-7-O-rutinoside (scolymoside); (6):Luteolin-7-O-glucoside;
(7):
Dicaffeoylquinic acid; (8): Dicaffeoylquinic acid (isomer I); (9): Dicaffeoylquinic acid (isomer); (10): 3-pCoumaoyl-4-caffeoylquinic acid; (11): 3-p-Coumaoyl-4-caffeoylquinic acid (isomer); (12): Dihydroxypropionhendhexoside; (13): Trihydroxyoctadecenoic acid.
Chlorogenic Acid vs Statins
Chlorogenic Acid
Simvastatin
Mevalonic acid
Hydoxycinnamates amount and…
µg/g
1200
1000
800
600
400
µg/g
200
0
Antioxidant activity
25
μmolTE/100g
20
15
10
5
0
μmolTE/100g
Chlorogenic acid:
Artichoke vs other vegetables
mg/100g
30
25
20
peach
apricot
15
nectarine
artichoke, edible portion
artichoke stems
10
5
0
peach
apricot
nectarine
artichoke, edible portion
artichoke stems
Artichoke Nutraceutic Market
Artichoke Nutraceutic Market
Conclusion
The research demonstrates how one can get from the
residues from the plant as a source of nutraceutical
molecules that can be used in medicine initiative.
If you reached the ultimate goal, this will involve:
• Reduction of welfare costs;
• Reducing the environmental impact of waste;
• Stimulus to the primary producers to obtain high quality
of vegetables;
• Revaluation of agricultural land otherwise depressed.
Il Carciofo dal tenero cuore si vestì da guerriero,
ispida edificò una piccola cupola, si mantenne
all’asciutto sotto le sue squame…
The Artichoke by
tender heart dressed
as a warrior
Shaggy built a small
dome, remained dry
under its scales ...
da “Ode al carciofo”